Application of near infra-red laser light increases current threshold in optic nerve consistent with increased Na < sup > + < /sup > -dependent transport
Pflugers Arch. 2024 Feb 29. doi: 10.1007/s00424-024-02932-1. Online ahead of print.ABSTRACTIncreases in the current threshold occur in optic nerve axons with the application of infra-red laser light, whose mechanism is only partly understood. In isolated rat optic nerve, laser light was applied near the site of electrical stimulation, via a flexible fibre optic. Paired applications of light produced increases in threshold that were reduced on the second application, the response recovering with increasing delays, with a time constant of 24 s. 3-min duration single applications of laser light gave rise to a rapid increase i...
Source: Pflugers Archiv : European Journal of Physiology - February 29, 2024 Category: Physiology Authors: Hin Heng Lo Tawan Munkongcharoen Rosa M Muijen Ritika Gurung Anjali G Umredkar Mark D Baker Source Type: research

Application of near infra-red laser light increases current threshold in optic nerve consistent with increased Na < sup > + < /sup > -dependent transport
Pflugers Arch. 2024 Feb 29. doi: 10.1007/s00424-024-02932-1. Online ahead of print.ABSTRACTIncreases in the current threshold occur in optic nerve axons with the application of infra-red laser light, whose mechanism is only partly understood. In isolated rat optic nerve, laser light was applied near the site of electrical stimulation, via a flexible fibre optic. Paired applications of light produced increases in threshold that were reduced on the second application, the response recovering with increasing delays, with a time constant of 24 s. 3-min duration single applications of laser light gave rise to a rapid increase i...
Source: Pflugers Archiv : European Journal of Physiology - February 29, 2024 Category: Physiology Authors: Hin Heng Lo Tawan Munkongcharoen Rosa M Muijen Ritika Gurung Anjali G Umredkar Mark D Baker Source Type: research

Application of near infra-red laser light increases current threshold in optic nerve consistent with increased Na < sup > + < /sup > -dependent transport
Pflugers Arch. 2024 Feb 29. doi: 10.1007/s00424-024-02932-1. Online ahead of print.ABSTRACTIncreases in the current threshold occur in optic nerve axons with the application of infra-red laser light, whose mechanism is only partly understood. In isolated rat optic nerve, laser light was applied near the site of electrical stimulation, via a flexible fibre optic. Paired applications of light produced increases in threshold that were reduced on the second application, the response recovering with increasing delays, with a time constant of 24 s. 3-min duration single applications of laser light gave rise to a rapid increase i...
Source: Pflugers Archiv : European Journal of Physiology - February 29, 2024 Category: Physiology Authors: Hin Heng Lo Tawan Munkongcharoen Rosa M Muijen Ritika Gurung Anjali G Umredkar Mark D Baker Source Type: research

Crystal structure and Hirshfeld surface analysis of a salt of antineoplastic kinase inhibitor vandetanib
A salt of vandetanib, namely, 4-({4-[(4-bromo-2-fluorophenyl)amino]-6-methoxyquinazolin-7-yl}methoxy)-1-methylpiperazin-1-ium 2-(butylamino)-4-phenoxy-6-sulfamoylbenzoate acetonitrile monosolvate, C22H25BrFN4O2+ · C17H19N2O5S − · C2H3N, composed of kinase inhibitor vandetanib and sulfamyl diuretic bumetanide in a 1:1 molar ratio, is reported. There is proton transfer between the piperidine ring of vandetanib and the carboxyl group of bumetanide to form the salt. In the vandetanib cation, the arene and pyrimidine rings are not coplanar, their planes subtending a dihedral angle of 60.47   (14) ° . The roles of the int...
Source: Acta Crystallographica Section C - February 7, 2024 Category: Chemistry Authors: Yang, H. Liang, M. Tian, F. Tags: Hirshfeld surface analysis salt vandetanib bumetanide crystal structure intermolecular interaction antineoplastic kinase inhibitor sulfamyl diuretic research papers Source Type: research

GSE254742 Sildenafil as a candidate drug for Alzheimer ’s disease: Real-world patient data observation and mechanistic observations from patient-induced pluripotent stem cell-derived neurons.
Contributors : Dhruv Gohel ; Amit K Gupta ; Feixiong ChengSeries Type : Expression profiling by high throughput sequencingOrganism : Homo sapiensAlzheimer ’s disease (AD) is a chronic neurodegenerative disease needing effective therapeutics urgently. Sildenafil, one of the approved phosphodiesterase-5 inhibitors, has been implicated as having potential beneficial effect in AD. We showed that sildenafil usage is associated with reduced likelihood of AD across four new drug compactor cohorts, including bumetanide, furosemide, spironolactone, and nifedipine. For instance, sildenafil usage is associated with a 54% reduced ...
Source: GEO: Gene Expression Omnibus - February 5, 2024 Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Homo sapiens Source Type: research

Liquid chromatography-tandem mass spectrometry determination of bumetanide in human plasma and application to a clinical pharmacokinetic study
This study aimed to develop and validate a specific, simple, sensitive, and accurate method using liquid chromatography-tandem mass spectrometry (LC-MS) for measuring bumetanide (BUM) in human plasma. Chromatographic separation was achieved using a Hypurity C18 column (4.6 × 50 mm, 5 μm) under isocratic conditions, and LC-MS detected positive ionization acquisition modes. Protonated precursor to product ion transitions were observed at m/z 365.08 → 240.10 and 370.04 → 244.52 for BUM and internal standard, respectively. The linear range of BUM in plasma samples was 3.490-401.192 ng/mL. The inter-precision value ranged...
Source: Biomedical Chromatography : BMC - January 18, 2024 Category: Biomedical Science Authors: Ganesan Padmini Tamilarasi Krishnan Manikandan Viswas Raja Solomon Source Type: research

Crossover randomized controlled trial of Bumetanide to rescue an attack of exercise induced hand weakness in Hypokalaemic Periodic Paralysis
Hypokalaemic periodic paralysis (HypoPP) is a neuromuscular disorder caused by mutations in the voltage-gated skeletal muscle channel genes CACNA1S and SCN4A. The genetic changes result in an aberrant inward leak current across the sarcolemma, which increases the susceptibility of the muscle membrane to sustained depolarisation at low serum potassium levels. Clinically this manifests as recurrent paralysis.[1] The only pharmacological option to abort acute symptoms in HypoPP is potassium supplementation. (Source: Neuromuscular Disorders)
Source: Neuromuscular Disorders - January 2, 2024 Category: Neurology Authors: Renata Siciliani Scalco, Jasper M Morrow, Andreea Manole, Iwona Skorupinska, Federico Ricciardi, Emma Matthews, Michael G Hanna, Doreen Fialho Source Type: research

Comparative Effect of Loop Diuretic Prescription on Mortality and Heart Failure Readmission
Loop diuretics are a standard pharmacologic therapy in heart failure (HF) management. Although furosemide is most frequently used, torsemide and bumetanide are increasingly prescribed in clinical practice, possibly because of superior bioavailability. Few real-world comparative effectiveness studies have examined outcomes across all 3 loop diuretics. The study goal was to compare the effects of loop diuretic prescribing at HF hospitalization discharge on mortality and HF readmission. We identified patients in Medicare claims data initiating furosemide, torsemide, or bumetanide after an index HF hospitalization from 2007 to...
Source: The American Journal of Cardiology - November 14, 2023 Category: Cardiology Authors: Arti V. Virkud, Patricia P. Chang, Michele Jonsson Funk, Abhijit V. Kshirsagar, Jessie K. Edwards, Virginia Pate, Michael R. Kosorok, Emily W. Gower Source Type: research

Anti-seizure medications for neonates with seizures
CONCLUSIONS: Phenobarbital as a first-line ASM is probably more effective than levetiracetam in achieving seizure control after the first loading dose and after the maximal loading dose of ASM (moderate-certainty evidence). Phenobarbital + bumetanide may have little or no difference in achieving seizure control when compared to phenobarbital alone (low-certainty evidence). Limited data and very low-certainty evidence preclude us from drawing any reasonable conclusion on the effect of using one ASM versus another on other short- and long-term outcomes. In neonates who achieve seizure control after the first loading dose of ...
Source: Cochrane Database of Systematic Reviews - October 24, 2023 Category: General Medicine Authors: Thangaraj Abiramalatha Sivam Thanigainathan Viraraghavan Vadakkencherry Ramaswamy Ronit Pressler Francesco Brigo Hans Hartmann Source Type: research

Anti-seizure medications for neonates with seizures
CONCLUSIONS: Phenobarbital as a first-line ASM is probably more effective than levetiracetam in achieving seizure control after the first loading dose and after the maximal loading dose of ASM (moderate-certainty evidence). Phenobarbital + bumetanide may have little or no difference in achieving seizure control when compared to phenobarbital alone (low-certainty evidence). Limited data and very low-certainty evidence preclude us from drawing any reasonable conclusion on the effect of using one ASM versus another on other short- and long-term outcomes. In neonates who achieve seizure control after the first loading dose of ...
Source: Cochrane Database of Systematic Reviews - October 24, 2023 Category: General Medicine Authors: Thangaraj Abiramalatha Sivam Thanigainathan Viraraghavan Vadakkencherry Ramaswamy Ronit Pressler Francesco Brigo Hans Hartmann Source Type: research

Compatibility of Omadacycline With Select Parenteral Products in Simulated Y-Site Administration
The objective of this work was to determine the intravenous compatibility of omadacycline with commonly used intravenous fluids and medications using simulated Y-site administration.METHODS: Omadacycline was prepared at concentrations consistent with a maintenance dose (1 mg/mL) and a loading dose (2 mg/mL) with 0.9% sodium chloride according to the prescribing information. Compatibility via simulated Y-site administration was assessed with selected crystalloids (lactated Ringer's solution, magnesium sulfate, and normal saline with potassium chloride) and intravenous medications (bumetanide, furosemide, heparin, and insuli...
Source: Clinical Therapeutics - September 30, 2023 Category: Drugs & Pharmacology Authors: David A Butler Kelly Moolick Donavon McCray Maxwell Gifford Source Type: research

Compatibility of Omadacycline With Select Parenteral Products in Simulated Y-Site Administration
The objective of this work was to determine the intravenous compatibility of omadacycline with commonly used intravenous fluids and medications using simulated Y-site administration.METHODS: Omadacycline was prepared at concentrations consistent with a maintenance dose (1 mg/mL) and a loading dose (2 mg/mL) with 0.9% sodium chloride according to the prescribing information. Compatibility via simulated Y-site administration was assessed with selected crystalloids (lactated Ringer's solution, magnesium sulfate, and normal saline with potassium chloride) and intravenous medications (bumetanide, furosemide, heparin, and insuli...
Source: Clinical Therapeutics - September 30, 2023 Category: Drugs & Pharmacology Authors: David A Butler Kelly Moolick Donavon McCray Maxwell Gifford Source Type: research

Effects of bumetanide on neonatal seizures: a systematic review of animal and human studies
Seizures are the most common neurological emergency in the neonatal period. They occur more often during the neonatal period than at any other time during life, with a reported incidence of one to five per 1,000 live births. [1] Phenobarbital is the first-line medication for neonatal seizures, other drugs being levetiracetam, phenytoin, midazolam, and lignocaine. [2,3] One recent pilot RCT found that 80% of infants who received phenobarbital remained seizure free for 24 hours [4] whereas the majority of studies have reported that currently used drugs achieve complete response only in 35-50% of cases after the initial loadi...
Source: Seizure: European Journal of Epilepsy - September 7, 2023 Category: Neurology Authors: Shripada Rao, Asifa Farhat, Abhijeet Rakshasbhuvankar, Sam Athikarisamy, Soumya Ghosh, Lakshmi Nagarajan Source Type: research

New GABA-Targeting Therapies for the Treatment of Seizures and Epilepsy: II. Treatments in Clinical Development
AbstractThe inhibitory neurotransmitter γ-aminobutyric acid (GABA) plays an important role in the modulation of neuronal excitability, and a disruption of GABAergic transmission contributes to the pathogenesis of some seizure disorders. Although many currently available antiseizure medications do act at least in part by potentiating GABA ergic transmission, there is an opportunity for further research aimed at developing more innovative GABA-targeting therapies. The present article summarises available evidence on a number of such treatments in clinical development. These can be broadly divided into three groups. The firs...
Source: CNS Drugs - August 21, 2023 Category: Neurology Source Type: research

Sub-dose anesthetics combined with chloride regulators protect the brain against chronic ischemia-hypoxia injury
CONCLUSION: Sub-anesthetic dose of propofol and sevoflurane is a recommended anesthesia regimen in at-risk patients. Restoration of [Cl- ]i homeostasis and GABAergic could further reduce the brain damage caused by ischemia-hypoxia.PMID:37545014 | DOI:10.1111/cns.14379 (Source: CNS Neuroscience and Therapeutics)
Source: CNS Neuroscience and Therapeutics - August 6, 2023 Category: Neuroscience Authors: Chenyi Yang Ye Wang Yun Li Xinyi Wang Wei Hua Zhuo Yang Haiyun Wang Source Type: research